Richard K. BRUICK,Charles G. CALDWELL,Doug E. FRANTZ,Kevin H. GARDNER,John B. MACMILLAN,Thomas H. SCHEUERMANN,Uttam K. TAMBAR
申请号:
US14442485
公开号:
US20160250216A1
申请日:
2013.11.14
申请国别(地区):
US
年份:
2016
代理人:
摘要:
Provided is a method of inhibiting heterodimerization of HIF-2α to HIF1β (ARNT) comprising binding certain small molecules to the HIF-2α PAS-B domain cavity but not to HIF1α and inhibiting HIF-2α heterodimerization to HIF1β (ARNT) but not inhibiting HIF1α heterodimerization to HIF1β (ARNT). Those certain small molecules are also referenced synonymously as HIF2-HDI and HIF2α heterodimerization inhibitors and also simply as certain small molecules.